Automated synthesis of heterocycles on solid supports.

Curr Opin Drug Discov Devel

Institut für Organische Chemie, Universität Karlsruhe (TH), D-76131 Karlsruhe, Germany.

Published: November 2006

The creation of novel diverse heterocycle libraries is an indispensable requirement of modern drug discovery processes. Currently, library sizes of over 10,000 discrete compounds are viable using programmed synthesis on solid supports. This review discusses the recent advances in the automated solid-phase syntheses of heterocycles to generate libraries of bioactive products, and illustrates library sizes that have been obtained, robots used for production of libraries, points of diversity and number of steps on the resin.

Download full-text PDF

Source

Publication Analysis

Top Keywords

solid supports
8
library sizes
8
automated synthesis
4
synthesis heterocycles
4
heterocycles solid
4
supports creation
4
creation novel
4
novel diverse
4
diverse heterocycle
4
heterocycle libraries
4

Similar Publications

Background: Predicting response to targeted cancer therapies increasingly relies on both simple and complex genetic biomarkers. Comprehensive genomic profiling using high-throughput assays must be evaluated for reproducibility and accuracy compared with existing methods.

Methods: This study is a multicenter evaluation of the Oncomine™ Comprehensive Assay Plus (OCA Plus) Pan-Cancer Research Panel for comprehensive genomic profiling of solid tumors.

View Article and Find Full Text PDF

Catalyst-Free Nitrogen Fixation by Microdroplets through a Radical-Mediated Disproportionation Mechanism under Ambient Conditions.

J Am Chem Soc

January 2025

State Key Laboratory of Physical Chemistry of Solid Surfaces, iChEM, College of Chemistry and Chemical Engineering, Innovation Laboratory for Sciences and Technologies of Energy Materials of Fujian Province (IKKEM), Xiamen University, Xiamen 361005, China.

Nitrogen fixation is essential for the sustainable development of both human society and the environment. Due to the chemical inertness of the N≡N bond, the traditional Haber-Bosch process operates under extreme conditions, making nitrogen fixation under ambient conditions highly desirable but challenging. In this study, we present an ultrasonic atomizing microdroplet method that achieves nitrogen fixation using water and air under ambient conditions in a rationally designed sealed device, without the need for any catalyst.

View Article and Find Full Text PDF

Diagnosis of Autism Spectrum Disorder (ASD) by Dynamic Functional Connectivity Using GNN-LSTM.

Sensors (Basel)

December 2024

College of Information Science and Engineering, Hunan Normal University, Changsha 410081, China.

Early detection of autism spectrum disorder (ASD) is particularly important given its insidious qualities and the high cost of the diagnostic process. Currently, static functional connectivity studies have achieved significant results in the field of ASD detection. However, with the deepening of clinical research, more and more evidence suggests that dynamic functional connectivity analysis can more comprehensively reveal the complex and variable characteristics of brain networks and their underlying mechanisms, thus providing more solid scientific support for computer-aided diagnosis of ASD.

View Article and Find Full Text PDF

The liver is supplied by a dual blood flow system consisting of the portal vein and hepatic artery. Imaging techniques for diagnosing hepatocellular carcinoma (HCC) have been developed along with blood flow imaging, which visualizes the amount of arterial and portal blood flow. The diagnosis of HCC differentiation is important for early-stage liver cancer screening and determination of treatment strategies.

View Article and Find Full Text PDF

Targeting Asparagine Metabolism in Solid Tumors.

Nutrients

January 2025

Department of Gastrointestinal Surgery, Graduate School of Medicine, Kyoto University, Kyoto 606-8507, Japan.

Reprogramming of energy metabolism to support cellular growth is a "hallmark" of cancer, allowing cancer cells to balance the catabolic demands with the anabolic needs of producing the nucleotides, amino acids, and lipids necessary for tumor growth. Metabolic alterations, or "addiction", are promising therapeutic targets and the focus of many drug discovery programs. Asparagine metabolism has gained much attention in recent years as a novel target for cancer therapy.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!